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Obat anti inflamasi non steroid Nurina H, dr. Inflammation injurious stimulus inflammatory process noxious agents : Infection Antibodies Physical injuries.

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Presentation on theme: "Obat anti inflamasi non steroid Nurina H, dr. Inflammation injurious stimulus inflammatory process noxious agents : Infection Antibodies Physical injuries."— Presentation transcript:

1 Obat anti inflamasi non steroid Nurina H, dr

2 Inflammation injurious stimulus inflammatory process noxious agents : Infection Antibodies Physical injuries CalorDolor RuborTumor Functiolesa Phase : acutesubacute chronic proliferative inflammatory response Essential for survival in the face of environmental pathogens and injury may be exaggerated & sustained without apparent benefit & w/ severe adverse consequences

3 Inflammation Therapeutic Strategies Relief of pain Slowing or-in theory-arrest of the tissue damaging process

4 NSAIDS: NONSTEROIDAL ANTIINFLAMMATORY DRUGS Chemistry & Pharmacokinetics Grouped in several chemical classes Varied pharmacokinetic characteristics But NSAIDs have some general properties in common

5 Chemistry & Pharmacokinetics NSAIDS: NONSTEROIDAL ANTIINFLAMMATORY DRUGS Weak organic acids except nabumetone Most are well absorbed Food doesn’t substantially change bioavalability Most are highly metabolized : phase I & II ; phase II alone Elimination : most important route – renal excretion nearly all undergo enterohepatic circulation Most are highly protein bound, usually to albumin

6 PHARMACODYNAMICS NSAIDS: NONSTEROIDAL ANTIINFLAMMATORY DRUGS antiinflammatory analgesicantipyretic Inhibition of Prostaglandin Biosynthesis Except paracetamol w/ very low anti inflammatory effect

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8 Cyclooxygenase (COX) 2 forms : cyclooxygenase-1 (COX-1) cyclooxygenase-2 (COX-2) 2 forms : cyclooxygenase-1 (COX-1) cyclooxygenase-2 (COX-2) COX-1 : primarily constitutive isoform COX-1 : primarily constitutive isoform found in most normal cells and tissues – kidney, GIT, platelet homeostasis COX-2 : induced during inflammation; facilitate the inflammatory response COX-2 : induced during inflammation; facilitate the inflammatory response

9 Origin & Effects of Prostaglandin

10 Classification of NSAIDs I. NON SELECTIVE COX INHIBITORS 1. SALICYLIC ACID DERIVATIVES - ASPIRIN, SODIUM SALICYLATE, SALSALATE, - ASPIRIN, SODIUM SALICYLATE, SALSALATE, 2. PARA – AMINOPHENOL DERIVATIVES - ACETAMINOPHEN ( PARACETAMOL ) - ACETAMINOPHEN ( PARACETAMOL ) 3. INDOLE & INDENE ACETIC ACIDS - INDOMETHACIN, SULINDAC - INDOMETHACIN, SULINDAC 4. HETEROARYL ACETIC ACIDS - TOL METIN, DICLOFENAC, KETOROLAC - TOL METIN, DICLOFENAC, KETOROLAC

11 Classification of NSAIDs - cont 5. ARYL PROPIONIC ACIDS -IBUPROFEN, NAPROXEN, FLURBIPROFEN, KETOPROFEN, FENOPROFEN, OXAPROZIN 6. ANTHRANILIC ACIDS ( FENAMATES ) - MEFENAMIC ACID, MECLOFENAMIC ACID 7. ENOLIC ACIDS - OXICAM ( PIROXICAM, MELOXICAM ) - OXICAM ( PIROXICAM, MELOXICAM ) 8. ALKANONES - NABUMETONE

12 Classification of NSAIDs - cont IISELECTIVE COX – 2 INHIBITOR 1. DIARYL – SUBTITUTED FURANONES -ROFECOXIB 2. DIARYL – SUBTITUTED PYRAZOLES - CELECOXIB 3. INDOLE ACETIC ACIDS - ETODOLAC 4. SULFONANILIDES - NIMESULIDE

13 Clinical uses of NSAIDs For analgesia (e.g. headache, dysmenorrhoea, backache, bony metastases, postoperative pain) For analgesia (e.g. headache, dysmenorrhoea, backache, bony metastases, postoperative pain) For anti-inflammatory effects (e.g. rheumatoid arthritis and related connective tissue disorders, gout and soft tissue disorders) For anti-inflammatory effects (e.g. rheumatoid arthritis and related connective tissue disorders, gout and soft tissue disorders) To lower temperature (antipyretic) To lower temperature (antipyretic)

14 NSAIDs: group-specific adverse effects

15 Adverse Effects of NSAID Therapy Gastrointestinal : anorexia, nausea, dyspepsia, abdominal pain, diarrhea Gastrointestinal : anorexia, nausea, dyspepsia, abdominal pain, diarrhea → gastric or intestinal ulcers ( ↓ with COX- 2-selective drugs) Cardiovascular : Cardiovascular : COX-2-selective- ↑ risk of heart attack and stroke COX-2-selective- ↑ risk of heart attack and stroke Analgesic Nephropathy Analgesic Nephropathy

16 Adverse Effects of NSAID Therapy Pregnancy : Prolongation of gestation, postpartum hemorrhage, closure of the ductus arteriosus and impaired fetal circulation in utero Pregnancy : Prolongation of gestation, postpartum hemorrhage, closure of the ductus arteriosus and impaired fetal circulation in utero Hypersensitivity: bronchial asthma, urticaria, shock Hypersensitivity: bronchial asthma, urticaria, shock Platelets: ↑ risk of hemorrhage Platelets: ↑ risk of hemorrhage Cox -2 selective- ↑ risk of thrombosis

17 Aspirin (acetylsalicylic acid) the oldest NSAID the oldest NSAID Is given orally and is rapidly absorbed; 75% is metabolised in the liver Is given orally and is rapidly absorbed; 75% is metabolised in the liver Also inhibits platelet aggregation → ↓ CHD Also inhibits platelet aggregation → ↓ CHD Unwanted effects : gastric bleeding; dizziness, deafness and tinnitus ('salicylism‘); postviral encephalitis (Reye's syndrome) in children; respiratory alkalosis followed by metabolic acidosis Unwanted effects : gastric bleeding; dizziness, deafness and tinnitus ('salicylism‘); postviral encephalitis (Reye's syndrome) in children; respiratory alkalosis followed by metabolic acidosis

18 Paracetamol/Acetaminophen potent analgesic and antipyretic actions but rather weaker anti-inflammatory effects potent analgesic and antipyretic actions but rather weaker anti-inflammatory effects administered orally administered orally mild to moderate pain: headache, mild to moderate pain: headache, myalgia, postpartum pain preferred to aspirin in children with viral infections preferred to aspirin in children with viral infections

19 Paracetamol/Acetaminophen Adverse Effects Adverse Effects therapeutic doses → a mild increase in hepatic enzymes larger doses → dizziness, excitement, disorientation 15 g → severe hepatotoxicity; acute renal tubular necrosis

20 DIPIRON analgesic +, antipyretic +, anti inflammatory – (weak) analgesic +, antipyretic +, anti inflammatory – (weak) Administered orally; parenteral Administered orally; parenteral Adverse Effects : agranulositosis, anemia aplastik, trombositopeni, hemolisis Adverse Effects : agranulositosis, anemia aplastik, trombositopeni, hemolisis

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